Generation of Endosomolytic Reagents by Branching of Cell-Penetrating Peptides: Tools for the Delivery of Bioactive Compounds to Live Cells in Cis or Trans

We describe the synthesis and cellular delivery properties of multivalent and branched delivery systems consisting of cell-penetrating peptides assembled onto a peptide scaffold using native chemical ligation. A trimeric delivery system presenting three copies of the prototypical cell-penetrating pe...

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Bibliographic Details
Published in:Bioconjugate chemistry 2010-12, Vol.21 (12), p.2164-2167
Main Authors: Angeles-Boza, Alfredo M., Erazo-Oliveras, Alfredo, Lee, Ya-Jung, Pellois, Jean-Philippe
Format: Article
Language:English
Subjects:
Amino Acid Sequence
Biological Products - chemistry
Biological Products - metabolism
Biological Products - pharmacology
Cell Membrane - metabolism
Cell-Penetrating Peptides - chemistry
Cell-Penetrating Peptides - metabolism
Cell-Penetrating Peptides - pharmacology
Drug Delivery Systems - methods
Endocytosis
Endosomes - drug effects
Endosomes - metabolism
Female
Fluorescein - metabolism
HeLa Cells
Humans
Polymers - chemistry
Polymers - metabolism
Polymers - pharmacology
Spectrometry, Fluorescence
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Summary:We describe the synthesis and cellular delivery properties of multivalent and branched delivery systems consisting of cell-penetrating peptides assembled onto a peptide scaffold using native chemical ligation. A trimeric delivery system presenting three copies of the prototypical cell-penetrating peptide TAT shows an endosomolytic activity much higher than its monomeric and dimeric counterparts. This novel reagent promotes the endosomal release of macromolecules internalized into cells by endocytosis, and as a result, it can be used to achieve cytosolic delivery of bioactive but cell-impermeable macromolecules in either cis (covalent conjugation) or trans (simple coincubation).
ISSN:1043-1802
1520-4812
DOI:10.1021/bc100130r